1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. GABA Receptor
    Cytochrome P450
  3. Clomethiazole

Clomethiazole 

Cat. No.: HY-129105 Purity: 98.19%
Handling Instructions

Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.

For research use only. We do not sell to patients.

Clomethiazole Chemical Structure

Clomethiazole Chemical Structure

CAS No. : 533-45-9

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Based on 1 publication(s) in Google Scholar

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Description

Chlormethiazole is an potent and orally active GABAA agonist[1]. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus[2].

In Vitro

Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1].
Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells, with EC50 values of 0.3 and 1.5 mM, respectively[1].
Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current[1].
Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 with IC50 values of 24 µM and 42 µM, respectively, in human liver microsomes, meanwhile all other isoforms exhibiting values > 300 µM[2].

Clinical Trial
Molecular Weight

161.65

Formula

C₆H₈ClNS

CAS No.

533-45-9

SMILES

CC1=C(CCCl)SC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

ClomethiazoleGABA ReceptorCytochrome P450Gamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCYPsanticonvulsantsedativeneuroprotectiveinsomniaalcoholismInhibitorinhibitorinhibit

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Clomethiazole
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HY-129105
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